Reaction Details |
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Target | Glucagon receptor |
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Ligand | BDBM50393781 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_857260 (CHEMBL2160605) |
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IC50 | 2.5±n/a nM |
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Citation | Xiong, Y; Guo, J; Candelore, MR; Liang, R; Miller, C; Dallas-Yang, Q; Jiang, G; McCann, PE; Qureshi, SA; Tong, X; Xu, SS; Shang, J; Vincent, SH; Tota, LM; Wright, MJ; Yang, X; Zhang, BB; Tata, JR; Parmee, ER Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes. J Med Chem55:6137-48 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glucagon receptor |
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Name: | Glucagon receptor |
Synonyms: | GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR) |
Type: | Enzyme |
Mol. Mass.: | 54026.92 |
Organism: | Homo sapiens (Human) |
Description: | P47871 |
Residue: | 477 |
Sequence: | MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ
CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL
FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC
WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN
MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV
HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
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BDBM50393781 |
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n/a |
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Name | BDBM50393781 |
Synonyms: | CHEMBL2159337 |
Type | Small organic molecule |
Emp. Form. | C32H24Cl2F3N3O4 |
Mol. Mass. | 642.452 |
SMILES | C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(cc1-c1ccc2cc(OC(F)(F)F)ccc2c1)-c1cc(Cl)cc(Cl)c1 |r| |
Structure |
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